ORALLY ADMINISTERED IRINOTECAN HC1 IN PATIENTS W/ ADVANCED SOLID TUMORS

晚期实体瘤患者口服伊立替康 HC1

• 批准号: 6264984
• 负责人: H PITOT
• 金额: $ 2.01万
• 依托单位: MAYO CLINIC ROCHESTER
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-12-01 至 1999-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6264984
• 关键词: clinical research; clinical trial phase I; dosage; drug screening /evaluation; human subject; human therapy evaluation; irinotecan; neoplasm /cancer; neoplasm /cancer chemotherapy; oral administration; pharmacokinetics

Irinotecan (CPT-11) is a semisynthetic derivative of camptothecin which acts by inhibiting topoisomerase I. It is our hypothesis that orally administered irinotecan HC1 (CPT-11) is a potent and effective antitumor agent. We are undertaking a phase I trial of oral irinotecan HC1 (CPT-11) in patients with advanced solid tumors. The objectives of the trial are: 1) to determine the MTD and the DLT of CPT-11 when administered orally once per day for five consecutive days every three weeks, 2) to define the safety profile of CPT-11 when administered orally on this schedule, 3) to characterize the single- and multiple-dose pharmacokinetics of CPT-11 and its metabolites, SN-38 and SN-38 glucuronide (SN-38G), and 4) to detect any evidence of antitumor activity. The current trial is very early in the accrual stage with a total of six patients enrolled at two different dose levels. Pharmacokinetic sampling is being performed on days one and five of cycle one. The study drug is being supplied by Pharmacia and Upjohn. Plans for future studies are pending at this time.

伊立替康（CPT-11）是喜树碱的半合成衍生物，通过抑制拓扑异构酶I发挥作用。我们假设口服给药的盐酸伊立替康（CPT-11）是一种强效且有效的抗肿瘤剂。 我们正在进行一项口服盐酸伊立替康（CPT-11）治疗晚期实体瘤患者的I期试验。 试验的目的是：1）确定CPT-11每3周一次，每天一次，连续5天口服给药时的MTD和DLT，2）确定CPT-11按该方案口服给药时的安全性特征，3）表征CPT-11及其代谢产物SN-38和SN-38葡糖苷酸（SN-38 G）的单次和多次给药药代动力学，和4）检测抗肿瘤活性的任何证据。 目前的试验处于招募阶段的早期，共有6名患者在两个不同的剂量水平下入组。 在第1周期的第1天和第5天进行药代动力学采样。 研究药物由Pharmacia和Upjohn提供。目前正在制定今后的研究计划。